Search Results
264 items found for "IJzerman AP"
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral membrane and regulates epithelial apicobasal The cleavage appears to occur at an atypical GPCR proteolysis site within the GAIN domain during an early Thus, the basolateral protein GPR125, an autocleavable adhesion GPCR, appears to play a crucial role in apicobasal polarization in epithelial cells."
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
They have participated in various cellular processes such as cell proliferation, migration, apoptosis
- Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation tailored specificities may expand the impact of these tools for both basic science and therapeutic applications
- Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
Here, ensemble refinement (ER) of crystallographic structures is applied to explore the impact of binding
- ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to the...
Overall, the comprehensive application of bioinformatics tools showed that functional mutations in the
- Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
PI3K/AKT/GSK-3β and MEK/ERK pathways in amygdalae of male mice, implicating a potential, therapeutic application
- GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...
This approach can expand the repertoire of adenosine receptor antagonists that can be designed based
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
been reached with therapies based on the GLP-1 receptor monoagonism; therefore, a logical and rational approach
- N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
Experimental approach: COS-7 cells were transfected with the human GLP-2R and assessed for cAMP accumulation
- Design and validation of recombinant protein standards for quantitative Western blot analysis of...
methods "Background: Replacement of radioligand binding assays with antibody-antigen interaction-based approaches
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
Moreover, molecular docking was applied to valid the important interactions between the ingredients and was involved in the biological process of GPCR signal transduction, hormone metabolism and nerve cell apoptosis
- Activation of GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through...
SIGNIFICANCE STATEMENT: Using a multi-disciplinary approach, we have characterized the molecular mechanisms
- Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist...
Using site-directed mutagenesis and species-swapping approaches, we identified key conserved amino acids
- Adenosine receptor signalling in Alzheimer's disease
Although there are no available medicines targeting these receptors approved for treating dementia, we
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
Remarkably, a significant part of the bound ligands appears exposed to the membrane lipids. The experimental structures do not usually account for the surrounding lipids, and their apparent contribution
- GPR15 expressed in T lymphocytes from RA patients is involved in leukocyte chemotaxis to the...
suggest that GPR15/GPR15L have a pathogenic role in RA and their antagonizing could be a therapeutic approach
- Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused...
unexpectedly showed no other autoimmune diseases, (d) showed spontaneously fluctuating Ca levels from approximately
- Co-activation of GPCRs facilitate GIRK-dependent current
The present study examined the interaction between D2 and GABAB receptors using transient applications of sub-saturating concentrations of agonists where the co-application of one agonist resulted in both
- G protein-coupled receptor signaling: transducers and effectors
a wide range of physiological functions and in a large number of Food and Drug Administration (FDA)-approved As new technologies are developed and applied to studying GPCR structure and their downstream effectors , there is increasing appreciation for the elegance of the regulatory mechanisms that mediate intracellular
- G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..
Aβ levels and leads to a decrease in the area and compaction of amyloid plaques in the preclinical AppNL-G-F
- Label-free LC-MS based assay to characterize small molecule compound binding to cells
This assay was applied to various target classes, with particular emphasis on those for which protein-based In another example, this assay was applied to an ion channel target with its agonists, of which the determined
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory However, until recently, most CB2 ligands were highly lipophilic and as such not optimal for clinical application A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties
- Bell-Evans model and steered molecular dynamics in uncovering the dissociation kinetics of ligands..
Non-equilibrium molecular simulation approaches are proven to be useful in this purpose. Here, we have implemented an optimized approach of combining the data derived from steered molecular Our results build a strong foundation for further improvement of our approach by rationalizing the kinetics
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory However, until recently, most CB2 ligands were highly lipophilic and as such, not optimal for clinical application A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties
- Community guidelines for GPCR ligand bias: IUPHAR review 32
2022 "GPCRs modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved
- Molecular insights into psychedelic drug action
drugs such as lysergic acid diethylamide (LSD), mescaline, and psilocybin: the desire for additional approaches Essential to the further development of such applications, however, is a clearer understanding of how
- Molecular targets of psychedelic-induced plasticity
In the prospect of a psychedelic drug becoming again an approved treatment, much of these efforts have
- Adenosine receptor signalling in Alzheimer's disease
Although there are no available medicines targeting these receptors approved for treating dementia, we